Cilengitide - 10mM in DMSO, high purity , CAS No.188968-51-6

Item Number
C422313
Grouped product items
SKUSizeAvailabilityPrice Qty
C422313-1ml
1ml
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$241.90

Potent and selective inhibitor of integrins αvβ3and αvβ5

Basic Description

SynonymsNSC 707544 | DTXSID9044035 | c(RGDfMeV) | HY-16141 | 4EDF46E4GI | Cilengitide | Cilengitide [USAN:INN] | EMD121974 | EMD-121974 | HALOFANTRINE HYDROCHLORIDE [MART.] | Cyclo(L-arginylglycyl-L-aspartyl-D-phenylalanyl-N-methyl-L-valyl) | NCGC00386242-02 | AC
Specifications & PurityMoligand™, 10mM in DMSO
Biochemical and Physiological MechanismsPotent and selective inhibitor of integrinsαvβ3andαvβ5(IC50values are 4.1 and 70 nM, respectively). Exhibits ~10-fold selectivity over gpIIb/IIIa. Increases endothelial monolayer permeability. Also exhibits antiangiogenic activity.
Storage TempStore at -80°C
Shipped InIce chest + Ice pads
GradeMoligand™
Product Description

Cilengitide is a potent integrin inhibitor for αvβ3 receptor and αvβ5 receptor with IC50 of 4.1 nM and 79 nM, respectively; ~10-fold selectivity against gpIIbIIIa.

Product Properties

ALogP-1

Associated Targets(Human)

ITGB3 Tclin Integrin beta-3 (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ITGAV Tchem Integrin alpha-V (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MDM2 Tchem p53-binding protein Mdm-2 (4545 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U-87 MG (3946 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MDM4 Tchem Protein Mdm4 (729 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ITGB3 Tclin Integrin alpha-V/beta-3 (2708 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ITGB3 Tclin Integrin alpha-IIb/beta-3 (3481 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ITGB1 Tclin Integrin alpha-5/beta-1 (686 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ITGAV Tchem Integrin alpha-V/beta-5 (589 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ITGAV Tchem Integrin alpha-V/beta-6 (509 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ITGAV Tchem Integrin alpha-V/alpha-5 (6 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ITGB3 Tclin Integrin alpha-V/beta-3/alpha-V/beta-5 (8 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Human alphaherpesvirus 1 (11089 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 2-[(2S,5R,8S,11S)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-7-methyl-3,6,9,12,15-pentaoxo-8-propan-2-yl-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid
INCHI InChI=1S/C27H40N8O7/c1-15(2)22-25(41)33-17(10-7-11-30-27(28)29)23(39)31-14-20(36)32-18(13-21(37)38)24(40)34-19(26(42)35(22)3)12-16-8-5-4-6-9-16/h4-6,8-9,15,17-19,22H,7,10-14H2,1-3H3,(H,31,39)(H,32,36)(H,33,41)(H,34,40)(H,37,38)(H4,28,29,30)/t17-,18-,19+,22-/m0/s1
InChi Key AMLYAMJWYAIXIA-VWNVYAMZSA-N
Canonical SMILES CC(C)C1C(=O)NC(C(=O)NCC(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)CC(=O)O)CCCN=C(N)N
Isomeric SMILES CC(C)[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](C(=O)N1C)CC2=CC=CC=C2)CC(=O)O)CCCN=C(N)N
PubChem CID 176873
Molecular Weight 588.66

Certificates

Certificate of Analysis(COA)

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Related Documents

Citations of This Product

1. Ying Song, Chen Li, Yahan Fu, Qiu Xie, Jun Guo, Guangming Li, Huiwen Wu.  (2020)  Inward Tension of Talin and Integrin-related Osmotic Pressure are involved Synergetically in the Invasion and Metastasis of Non-small Cell Lung Cancer.  Journal of Cancer,  11  (17): ( 5032–5041).  [PMID:32742451]
2. Yifan Wang, Xiaolong Zhang, Jilai Tian, Jinjun Shan, Yunfeng Hu, Yiqian Zhai, Jun Guo.  (2019)  Talin promotes integrin activation accompanied by generation of tension in talin and an increase in osmotic pressure in neurite outgrowth.  FASEB JOURNAL,  33  (5): (6311-6326).  [PMID:30768370]
3. Siming Yu, Linna Li, Wei Tian, Dan Nie, Wei Mu, Fang Qiu, Yu Liu, Xinghan Liu, Xiaofeng Wang, Zhimin Du, Wen-Feng Chu, Baofeng Yang.  (2018)  PEP06 polypeptide 30 exerts antitumour effect in colorectal carcinoma via inhibiting epithelial–mesenchymal transition.  BRITISH JOURNAL OF PHARMACOLOGY,  175  (15): (3111-3130).  [PMID:29722931]

References

1. Ying Song, Chen Li, Yahan Fu, Qiu Xie, Jun Guo, Guangming Li, Huiwen Wu.  (2020)  Inward Tension of Talin and Integrin-related Osmotic Pressure are involved Synergetically in the Invasion and Metastasis of Non-small Cell Lung Cancer.  Journal of Cancer,  11  (17): ( 5032–5041).  [PMID:32742451]
2. Yifan Wang, Xiaolong Zhang, Jilai Tian, Jinjun Shan, Yunfeng Hu, Yiqian Zhai, Jun Guo.  (2019)  Talin promotes integrin activation accompanied by generation of tension in talin and an increase in osmotic pressure in neurite outgrowth.  FASEB JOURNAL,  33  (5): (6311-6326).  [PMID:30768370]
3. Siming Yu, Linna Li, Wei Tian, Dan Nie, Wei Mu, Fang Qiu, Yu Liu, Xinghan Liu, Xiaofeng Wang, Zhimin Du, Wen-Feng Chu, Baofeng Yang.  (2018)  PEP06 polypeptide 30 exerts antitumour effect in colorectal carcinoma via inhibiting epithelial–mesenchymal transition.  BRITISH JOURNAL OF PHARMACOLOGY,  175  (15): (3111-3130).  [PMID:29722931]

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